Assay Detail
Binding
CHEMBL4704017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay
19
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of OATD-01, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.37 | 8.80 |
| Ki | 1 | 8.32 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4756869 | — | — | 1 | 8.80 |
| CHEMBL4794014 | — | — | 1 | 8.47 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | 2.0 | 2 | 8.32 |
| CHEMBL4789376 | — | — | 1 | 8.17 |
| CHEMBL4640857 | — | — | 1 | 8.15 |
| CHEMBL4764430 | — | — | 1 | 8.15 |
| CHEMBL4755139 | — | — | 1 | 8.05 |
| CHEMBL4076989 | — | — | 1 | 7.85 |
| CHEMBL4461925 | — | — | 1 | 7.66 |
| CHEMBL4580568 | — | — | 1 | 7.64 |
| CHEMBL4749391 | — | — | 1 | 7.62 |
| CHEMBL4776610 | — | — | 1 | 7.27 |
| CHEMBL4206372 | — | — | 1 | 7.08 |
| CHEMBL4209364 | — | — | 1 | 6.40 |
| CHEMBL4742167 | — | — | 1 | 6.08 |
| CHEMBL4791640 | — | — | 1 | 6.07 |
| CHEMBL4758240 | — | — | 1 | 5.89 |
| CHEMBL4758850 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4756869 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4794014 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4789376 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4640857 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4764430 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4755139 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4788866 | 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4076989 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL4461925 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4580568 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4749391 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4776610 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4206372 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4209364 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4742167 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4791640 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4758240 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4758850 | — | IC50 | = | 6400.0 | nM | 5.19 |